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Practical synthesis of hydroxychromenes and evaluation of their biological activity

Title
Practical synthesis of hydroxychromenes and evaluation of their biological activity
Authors
Jung J.-C.Oh S.
Ewha Authors
오세관
SCOPUS Author ID
오세관scopus
Issue Date
2012
Journal Title
Molecules
ISSN
1420-3049JCR Link
Citation
vol. 17, no. 1, pp. 240 - 247
Indexed
SCIE; SCOPUS WOS scopus
Abstract
A simple and efficient seven steps synthesis of brodifacoum and difethialone from phenylacetyl chloride is described. The key synthetic strategies involve Friedel-Crafts acylation, intramolecular ring cyclization and condensation reaction in the presence of Brønsted-Lowry acids. It was found that brodifacoum showed favorable inhibiting activities on LPS-stimulated nitrite production in BV-2 microglia cells. Brodifacoum exhibited superior anti-inflammatory effects than difethialone. We expect that an efficient linear synthesis of 4-hydroxycoumarin derivatives and key fragments that are useful agents for the modulation of inflammation as well as inhibition of coagulation will be of practical use. © 2012 by the authors.
DOI
10.3390/molecules17010240
Appears in Collections:
의학전문대학원 > 의학과 > Journal papers
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